W-7 

W-7 is a selective calmodulin antagonist. W-7 inhibits the Ca²⁺-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC₅₀ values of 28 μM and 51 μM, respectively. W-7 induces apoptosis and has antitumor and vascular relaxing activity. W-7 is a blocker of Kv4.3 and can be used for research of arrhythmias^{[1][2][3][4][5][6]}.

W-7 主要分布在细胞质中，并抑制中国仓鼠卵巢 K1 (CHO-K1) 细胞的增殖。W-7 以某种方式选择性地阻断细胞周期的阶段 (G1/S 边界阶段)。25 μM W-7 阻止在细胞周期的 G1/S 边界期的细胞的生长^[1]。
W-7 (100 μM) 对卡巴胆碱和氯化钾诱导的收缩反应表现出相似程度的拮抗作用。W-7 抑制肌球蛋白轻链 (P-LC) 磷酸盐含量增加以响应卡巴胆碱刺激 (10 μM 1 分钟)。W-7 通过抑制 P-LC 磷酸化来拮抗平滑肌收缩^[2]。
W-7 处理会剂量依赖性抑制各种人类多发性骨髓瘤细胞系增殖。W-7 通过下调细胞周期蛋白和上调 p21cip1 诱导 G1 期细胞周期停滞。W-7 通过 caspase 激活诱导细胞凋亡，并诱导细胞内钙水平升高和线粒体膜电位去极化，抑制 STAT3 磷酸化和随后的 Mcl-1 蛋白下调^[3]。
W-7 竞争性抑制 Ca²⁺/ 钙调蛋白依赖性磷酸二酯酶，K_i 值为 300 μM^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

W-7 (3 mg/kg；腹膜内注射；每周连续 5 天；雌性 BALB/c nu 小鼠) 处理可显著减少小鼠 MM 模型中的肿瘤生长^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

340.87

C₁₆H₂₁ClN₂O₂S

65595-90-6

固体

Light yellow to yellow

Room temperature in continental US; may vary elsewhere.

• [1]. H Hidaka, et al. N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide, a Calmodulin Antagonist, Inhibits Cell Proliferation. Proc Natl Acad Sci U S A. 1981 Jul;78(7):4354-7.  [Content Brief]

  [2]. M Asano. Divergent Pharmacological Effects of Three Calmodulin Antagonists, N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7), Chlorpromazine and Calmidazolium, on Isometric Tension Development and Myosin Light Chain Phosphorylation in Intact Bovine Tracheal Smooth Muscle. J Pharmacol Exp Ther. 1989 Nov;251(2):764-73.  [Content Brief]

  [3]. H Itoh, et al. Direct Interaction of Calmodulin Antagonists With Ca2+/calmodulin-dependent Cyclic Nucleotide Phosphodiesterase. J Biochem. 1984 Dec;96(6):1721-6.H Itoh, et al. Direct Interaction of Calmodulin Antagonists With Ca2+/calmodulin-dependent Cyclic Nucleotide Phosphodiesterase. J Biochem. 1984 Dec;96(6):1721-6.  [Content Brief]

  [4]. Shigeyuki Yokokura, et al. Calmodulin Antagonists Induce Cell Cycle Arrest and Apoptosis in Vitro and Inhibit Tumor Growth in Vivo in Human Multiple Myeloma. BMC Cancer. 2014 Nov 26;14:882.  [Content Brief]

  [5]. Qu YJ, et al. W-7 modulates Kv4.3: pore block and Ca2+-calmodulin inhibition. Am J Physiol Heart Circ Physiol. 2007 May;292(5):H2364-77.  [Content Brief]

  [6]. Gbadebo TD, et al. Calmodulin inhibitor W-7 unmasks a novel electrocardiographic parameter that predicts initiation of torsade de pointes. Circulation. 2002 Feb 12;105(6):770-4.  [Content Brief]